156273-72-2

Upstream product

• 156273-71-1 N-benzyl-(Z)-N'-(2-amino-1,2-dicyanovinyl)formamidine 
• 88333-03-3 Benzyl isocyanide 
• 129694-52-6 ethyl (Z)-N-(2-amino-1,2-dicyanovinyl)formamidate 
• 100-46-9 benzylamine 
• 133123-63-4 N-(2-amino-1,2-dicyano-vinyl)-formimydic acid ethyl ester 
• 906731-78-0 C₁₂H₁₁N₅ 

Downstream Products

• 156273-73-3 9-Benzyl-2,2-dimethyl-2,9-dihydro-1H-purine-6-carboxylic acid amide 
• 1421053-58-8 1-(4-methoxybenzyl)-4-(5-amino-1-benzyl-1H-imidazol-4-yl)-5-imino-1H-imidazol-2(5H)-one 
• 156273-81-3 5-amino-4--1-benzimidazole 
• 156273-83-5 5-amino-4--1-benzimidazole 
• 156273-80-2 5-acetamido-4-(C-cyanoformimidoyl)-1-benzylimidazole 

Relevant academic research and scientific papers

Structure-based drug design and potent anti-cancer activity of tricyclic 5:7:5-fused diimidazo[4,5-d:4′,5′-f][1,3]diazepines

Judicial structural modifications of 5:7-fused ring-expanded nucleosides (RENs), based on molecular modeling studies with one of its known targets, human RNA helicase (hDDX3), led to the lead, novel, 5:7-5-fused tricyclic heterocycle (1). The latter exhibited promising broad-spectrum in vitro anti-cancer activity against a number of cancer cell lines screened. This paper describes our systematic, albeit limited, structure-activity relationship (SAR) studies on this lead compound, which produced a number of analogs with broad-spectrum in vitro anti-cancer activities against lung, breast, prostate, and ovarian cancer cell lines, in particular compounds 15i, 15j, 15m and 15n which showed IC 50 values in submicromolar to micromolar range, and are worthy of further explorations. The SAR data also enabled us to propose a tentative SAR model for future SAR efforts for ultimate realization of optimally active and minimally toxic anti-cancer compounds based on the diimidazo[4,5-d:4′, 5′-f][1,3]diazepine structural skeleton of the lead compound 1.

Process for the production of pentostatin aglycone and pentostatin

A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available L-Dialkyl tartarates.

Synthesis of 4- and 5-disubstituted 1-benzylimidazoles, important precursors of purine analogs

(Z)-N-(2-amino-1,2-dicyanovinyl)-N'-benzylformamidine 6 has been prepared both from the reaction of benzylisonitrile with the hydrochloride salt of diaminomaleonitrile and from reaction of ethyl (Z)-N-(2-amino-1,2-dicyanovinyl)formimidate with benzylamine